Add to ORKGPeptide-derived protease inhibitors are an important class of compounds with the potential to treat a wide range of diseases. Herein, we describe the synthesis of a series of triazole- containing macrocyclic protease inhibitors pre-organized into a b-strand conformation and an evaluation of their activity against a panel of proteases. Acyclic azidoalkyne-based aldehydes are also evaluated for comparison. The macrocyclic peptidomimetics showed considerable activity towards calpain II, cathepsin L and S, and the 20S proteasome chymotrypsin-like activity. Some of the first examples of highly potent macrocyclic inhibitors of cathepsin S were identified. These adopt a well-defined b-strand geometry as shown by NMR spectroscopy, X-ray analysis, a...
Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the pe...
Seven novel tertiary alcohol containing linear HIV-1 protease inhibitors (PIs), decorated at the par...
The natural synthesis of peptides and proteins occurs in an efficient iterative manner, and can be c...
Peptide-derived protease inhibitors are an important class of compounds with the potential to treat ...
This research explores the first design and synthesis of macrocyclic peptide aldehydes as potent inh...
There is a real need for simple structures that define a β-strand conformation, a secondary structur...
This research explores the first design and synthesis of macrocyclic peptide aldehydes as potent inh...
Chapter One introduces the concept of peptide 'secondary structure' with an emphasis on β-strand geo...
The macrocyclization of linear peptides is very often accompanied by significant improvements in the...
Inhibition of a class of cysteine proteases known as the cathepsins has received increasing attentio...
Aza-peptide aldehydes and ketones are a new class of reversible protease inhibitors that are specifi...
Inhibition of the Keap1-Nrf2 protein-protein interaction (PPI) is thought to have therapeutic potent...
The study of protein mechanism and function is central to the development of biosensing tools and th...
New peptidic templates constrained into a β-strand geometry by linking acetylene and azide containin...
Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the pe...
Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the pe...
Seven novel tertiary alcohol containing linear HIV-1 protease inhibitors (PIs), decorated at the par...
The natural synthesis of peptides and proteins occurs in an efficient iterative manner, and can be c...
Peptide-derived protease inhibitors are an important class of compounds with the potential to treat ...
This research explores the first design and synthesis of macrocyclic peptide aldehydes as potent inh...
There is a real need for simple structures that define a β-strand conformation, a secondary structur...
This research explores the first design and synthesis of macrocyclic peptide aldehydes as potent inh...
Chapter One introduces the concept of peptide 'secondary structure' with an emphasis on β-strand geo...
The macrocyclization of linear peptides is very often accompanied by significant improvements in the...
Inhibition of a class of cysteine proteases known as the cathepsins has received increasing attentio...
Aza-peptide aldehydes and ketones are a new class of reversible protease inhibitors that are specifi...
Inhibition of the Keap1-Nrf2 protein-protein interaction (PPI) is thought to have therapeutic potent...
The study of protein mechanism and function is central to the development of biosensing tools and th...
New peptidic templates constrained into a β-strand geometry by linking acetylene and azide containin...
Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the pe...
Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the pe...
Seven novel tertiary alcohol containing linear HIV-1 protease inhibitors (PIs), decorated at the par...
The natural synthesis of peptides and proteins occurs in an efficient iterative manner, and can be c...